计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
利菲拉非尼（BGB-283）, 丝氨酸/苏氨酸蛋白激酶 B-raf 抑制剂
有货
概述
Information
Lifirafenib (BGB-283, Beigene-283) potently inhibitsRAFfamily kinases andEGFRactivities in biochemical assays withIC50values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.
In vitro
In vitro, BGB-283 potently inhibits BRAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAFV600E and EGFR mutation/amplification. In BRAFV600E colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. It demonstrates selective cytotoxicity to cell lines harboring BRAFV600E or EGFR mutations. BGB-283 inhibits the EGF-induced EGFR autophosphorylation on Tyr1068 in A431 cells in a dose-dependent manner. In WiDr colorectal cancer cells, BGB-283 is shown to be able to inhibit the feedback activation of EGFR signaling and achieves sustained inhibition of pERK.
In vivo
In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRAFV600E mutation. BGB-283 is highly efficacious in BRAF(V600E) colorectal cancer xenograft models, including HT29, Colo205, and two primary tumor xenografts harboring BRAFV600E mutation. In addition, BGB-283 shows compelling efficacy in a WiDr xenograft model where EGFR reactivation is shown to be induced upon BRAF inhibition. BGB-283 induces tumor regression in HCC827 but not in A431 xenograft. BGB-283 inhibits phosphorylation of both ERK1/2 and EGFR and displays potent antitumor activity in WiDr tumor xenografts. BGB-283 does not induce EGFR feedback activation as reported for vemurafenib. BGB-283 potently inhibits MEK and ERK phosphorylation and DUSP6 expression in vivo when dosed repeatedly. There is no detectable difference on AKT phosphorylation.
Cell Data
cell lines：
Concentrations：0.03, 1, 10 μM
Incubation Time：3 days
Powder Purity:≥99%
规格
英文别名
Beigene-283
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Lifirafenib (BGB-283)
生化机理
利非非尼（BGB-283，Beigene-283）在生化试验中能有效抑制 RAF 家族激酶和表皮生长因子受体的活性，对重组 BRAFV600E 激酶域、表皮生长因子受体和表皮生长因子受体 T790M/L858R 突变体的 IC50 值分别为 23、29 和 495 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
丝氨酸/苏氨酸蛋白激酶 B-raf 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CC(=O)NC2=NC=CC(=C21)OC3=CC4=C(C=C3)O[C@H]5[C@@H]4[C@@H]5C6=NC7=C(N6)C=C(C=C7)C(F)(F)F
分子量
478.42
Reaxy-Rn
23782872
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23782872&ln=
高级数据
产品属性
| IC50 | EGFR, IC50: 29 nM |
|---|
关联靶点（人）
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(1 活性数据)
BRAF
Tclin
丝氨酸/苏氨酸蛋白激酶B-raf(Serine/threonine-protein kinase B-raf)
(1 活性数据)
ARAF
Tchem
丝氨酸/苏氨酸蛋白激酶 A-Raf(Serine/threonine-protein kinase A-Raf)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 52 mg/mL (201.73 mM); Ethanol: 52 mg/mL (201.73 mM); DMSO: Insoluble;
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H302: 吞食有害
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P271: 仅在室外或通风良好的地方使用。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P330: 漱口
P302+P352: 如皮肤沾染：用水充分清洗。
P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。
P405: 密闭存放
P403+P233: 存放在通风良好的地方。保持容器密闭。
P501: 将内容物/容器送到批准的废物处理厂处理
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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危险品化学品经营许可证（带存储）